Methotrexate (MTX)

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General information

Class/mechanism: Folate analog, antimetabolite, interferes with DNA synthesis. Methotrexate inhibits dihydrofolic acid reductase, which catalyzes reactions that produce tetrahydrofolates, which are used in purine nucleotide and thymidylate synthesis.[1][2][3][4][5][6][7]
Route: IV, PO, IM, IT, SC, intraarterial
Extravasation: inflammitant

  • Glucarpidase (Voraxaze) can be used to treat toxic plasma methotrexate concentrations (greater than 1 micromole per liter) in patients with delayed methotrexate clearance due to impaired renal function

For conciseness and simplicity, currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.[1]

Diseases for which it is used

Patient drug information

History of changes in FDA indication

  • 12/7/1953: Initial FDA approval

Also known as

Abitrexate Alltrex Amethopterin Antifolan Artrait Biometrox Biotrexate Caditrex
Cytotrexate Ebetrexat Emthexat Emthexate Ervemin Farmitrexat Fauldmetro Folex PFS
Folitrax Hextrate Ifamet Imutrex Ledertrexate Ledertrexato Lumexon Matrex
Maxtrex Medsatrexate Merex Metex Methobax Methoblastin Methorex Methotrexaat
Methotrexat Methotrexato Methotrexatum Meticil Metolate Metotressato Metotrexate Metotrexato
Metotrexol Metrex Metrexan Metrexato Metrotex Mexate Miantrex CS MTX
Neometho Neotrexate Novatrex Oncotrex O Trexat Pharmatrexate Remtrex Reumatrex
Rextop Rheumatrex Tecnomet Texate Texorate Tratoben Tremetex Trexall
Trexan Trexeron Trixilem Unitrexate Zexate


  1. 1.0 1.1 Methotrexate (MTX) tablet package insert
  2. Methotrexate (MTX) tablet package insert (locally hosted backup)
  3. Methotrexate (MTX) injection package insert
  4. Methotrexate (MTX) injection package insert (locally hosted backup)
  5. 5.0 5.1 Methotrexate (Otrexup) subcutaneous injection package insert
  6. Methotrexate (Otrexup) subcutaneous injection package insert (locally hosted backup)
  7. Otrexup manufacturer's website
  8. Methotrexate (MTX) patient drug information (Chemocare)
  9. Methotrexate (MTX) patient drug information (UpToDate)